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Setipiprant
CAS No. 866460-33-5
Setipiprant ( ACT-129968 | ACT 129968 | KYTH 105 | Setipiprant )
产品货号. M19195 CAS No. 866460-33-5
Setipiprant 是一种口服的选择性 CRTH2 拮抗剂 (IC50: 6.0 nM)。 CRTH2 是前列腺素 (PGD2) 的 G 蛋白偶联受体。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥211 | 有现货 |
|
| 10MG | ￥316 | 有现货 |
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| 25MG | ￥583 | 有现货 |
|
| 50MG | ￥956 | 有现货 |
|
| 100MG | ￥1531 | 有现货 |
|
| 200MG | ￥2252 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称Setipiprant
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述Setipiprant 是一种口服的选择性 CRTH2 拮抗剂 (IC50: 6.0 nM)。 CRTH2 是前列腺素 (PGD2) 的 G 蛋白偶联受体。
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产品描述Setipiprant is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2 is a G protein-coupled receptor for prostaglandin (PGD2). PGD2 is produced by the mast cells and is a key mediator in various inflammatory diseases, including allergy and asthma. Binding of PGD2 to CRTH2, which are expressed on the surface of blood-borne cells, induces chemotaxis of Th2 cells, basophils, and eosinophils, and stimulates cytokine release from these cells.(In Vitro):Setipiprant (0-10 μM; 90 min) interacts with hCRTH2 receptor in the absence and presence of Human Serum Albumin (HSA) in the assay buffer with IC50 values of 6 and 340 nM, respectively.Setipiprant (0-10 μM; 5-20 min) inhibits hCRTH2 receptor based intracellular calcium liberation, intracellular cAMP and shape change of human eosinophils with IC50 values of 30, 80 and 235 nM, respectively.Setipiprant (0-10 μM) inhibits prostanoid receptors hDP1, hEP2 and hEP4 with IC50 values of 1290, 2600 and ＞10000 nM, respectively.(In Vivo):Pharmacokinetic Properties of Setipiprant in Rats and Dogs.
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体外实验Setipiprant (0-10 μM; 90 min) interacts with hCRTH2 receptor in the absence and presence ofHuman Serum Albumin (HSA) in the assay buffer with IC50 values of 6 and 340 nM, respectively.Setipiprant (0-10 μM; 5-20 min) inhibits hCRTH2 receptor based intracellular calcium liberation, intracellular cAMP and shape change of human eosinophils with IC50 values of 30, 80 and 235 nM, respectively.Setipiprant (0-10 μM) inhibits prostanoid receptors hDP1, hEP2 and hEP4 with IC50 values of 1290, 2600 and ＞10000 nM, respectively.
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体内实验——
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同义词ACT-129968 | ACT 129968 | KYTH 105 | Setipiprant
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通路Others
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靶点Other Targets
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受体CRTh2
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研究领域Inflammation/Immunology
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适应症——
化学信息
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CAS Number866460-33-5
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分子量402.42
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分子式C24H19FN2O3
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纯度>98% (HPLC)
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溶解度DMSO : ≥ 36 mg/mL; 89.46 mM
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SMILESC1CN(CC2=C1N(C3=C2C=C(C=C3)F)CC(=O)O)C(=O)C4=CC=CC5=CC=CC=C54
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化学全称2-(2-(1-naphthoyl)-8-fluoro-1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-5-yl)acetic acid
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Diamant Z., et al. Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug;44(8):1044-52.
产品手册
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